发明名称 兰索拉唑化合物
摘要 本发明属于医药技术领域,具体涉及右兰索拉唑化合物及其制备方法,本发明得到的化合物,含有两个半结晶水,具有的优点:化学纯度99.95%,最大杂质小于1‰,光学纯度高达99.99%ee;稳定性好。本发明还涉及使用这种化合物的组合物制造治疗非糜烂性胃食管反流引起的胃部灼热感、糜烂性食管炎药物中的应用。
申请公布号 CN102234265A 申请公布日期 2011.11.09
申请号 CN201110224746.7 申请日期 2011.08.08
申请人 天津市汉康医药生物技术有限公司 发明人 严洁;黄欣
分类号 C07D401/12(2006.01)I;A61K31/4439(2006.01)I;A61P1/04(2006.01)I 主分类号 C07D401/12(2006.01)I
代理机构 代理人
主权项 1.式Ⅰ所示右兰索拉唑化合物的水合物,<img file="2011102247467100001DEST_PATH_IMAGE001.GIF" wi="" he="" />(Ⅰ)用卡尔费休法测定,所述水合物含有10.78%—10.95%(重量百分比)的水分;所述右兰索拉唑水合物的晶体,用CuKa射线作为特征X射线粉末测定中,其图谱具有下列2θ衍射角和D值,<tables num="0001"><table><tgroup cols="4"><colspec colname="c001" colwidth="16%" /><colspec colname="c002" colwidth="31%" /><colspec colname="c003" colwidth="31%" /><colspec colname="c004" colwidth="20%" /><tbody><row><entry morerows="1">峰数</entry><entry morerows="1">2θ角(°)实测值</entry><entry morerows="1">d()实测值</entry><entry morerows="1">I/I<sub>0</sub></entry></row><row><entry morerows="1">1</entry><entry morerows="1">5.700</entry><entry morerows="1">15.4919</entry><entry morerows="1">18</entry></row><row><entry morerows="1">2</entry><entry morerows="1">9.860</entry><entry morerows="1">8.9632</entry><entry morerows="1">33</entry></row><row><entry morerows="1">3</entry><entry morerows="1">10.900</entry><entry morerows="1">8.1102</entry><entry morerows="1">9</entry></row><row><entry morerows="1">4</entry><entry morerows="1">11.400</entry><entry morerows="1">7.7556</entry><entry morerows="1">61</entry></row><row><entry morerows="1">5</entry><entry morerows="1">12.440</entry><entry morerows="1">7.1094</entry><entry morerows="1">78</entry></row><row><entry morerows="1">6</entry><entry morerows="1">13.980</entry><entry morerows="1">6.3295</entry><entry morerows="1">13</entry></row><row><entry morerows="1">7</entry><entry morerows="1">14.900</entry><entry morerows="1">5.9407</entry><entry morerows="1">32</entry></row><row><entry morerows="1">8</entry><entry morerows="1">16.100</entry><entry morerows="1">5.5005</entry><entry morerows="1">22</entry></row><row><entry morerows="1">9</entry><entry morerows="1">17.080</entry><entry morerows="1">5.1871</entry><entry morerows="1">61</entry></row><row><entry morerows="1">10</entry><entry morerows="1">17.280</entry><entry morerows="1">5.1275</entry><entry morerows="1">32</entry></row><row><entry morerows="1">11</entry><entry morerows="1">18.140</entry><entry morerows="1">4.8863</entry><entry morerows="1">7</entry></row><row><entry morerows="1">12</entry><entry morerows="1">18.860</entry><entry morerows="1">4.7014</entry><entry morerows="1">100</entry></row><row><entry morerows="1">13</entry><entry morerows="1">19.840</entry><entry morerows="1">4.4713</entry><entry morerows="1">33</entry></row><row><entry morerows="1">14</entry><entry morerows="1">20.420</entry><entry morerows="1">4.3456</entry><entry morerows="1">30</entry></row><row><entry morerows="1">15</entry><entry morerows="1">21.920</entry><entry morerows="1">4.0515</entry><entry morerows="1">11</entry></row><row><entry morerows="1">16</entry><entry morerows="1">23.080</entry><entry morerows="1">3.8504</entry><entry morerows="1">19</entry></row><row><entry morerows="1">17</entry><entry morerows="1">23.620</entry><entry morerows="1">3.7636</entry><entry morerows="1">88</entry></row><row><entry morerows="1">18</entry><entry morerows="1">24.480</entry><entry morerows="1">3.6333</entry><entry morerows="1">43</entry></row><row><entry morerows="1">19</entry><entry morerows="1">25.040</entry><entry morerows="1">3.5533</entry><entry morerows="1">21</entry></row><row><entry morerows="1">20</entry><entry morerows="1">26.140</entry><entry morerows="1">3.4062</entry><entry morerows="1">18</entry></row><row><entry morerows="1">21</entry><entry morerows="1">26.360</entry><entry morerows="1">3.3783</entry><entry morerows="1">22</entry></row><row><entry morerows="1">22</entry><entry morerows="1">27.040</entry><entry morerows="1">3.2948</entry><entry morerows="1">6</entry></row><row><entry morerows="1">23</entry><entry morerows="1">27.400</entry><entry morerows="1">3.2524</entry><entry morerows="1">36</entry></row><row><entry morerows="1">24</entry><entry morerows="1">28.300</entry><entry morerows="1">3.1509</entry><entry morerows="1">6</entry></row><row><entry morerows="1">25</entry><entry morerows="1">28.760</entry><entry morerows="1">3.1016</entry><entry morerows="1">18</entry></row><row><entry morerows="1">26</entry><entry morerows="1">29.000</entry><entry morerows="1">3.0764</entry><entry morerows="1">91</entry></row><row><entry morerows="1">27</entry><entry morerows="1">30.000</entry><entry morerows="1">2.9761</entry><entry morerows="1">11</entry></row><row><entry morerows="1">28</entry><entry morerows="1">30.500</entry><entry morerows="1">2.9285</entry><entry morerows="1">6</entry></row><row><entry morerows="1">29</entry><entry morerows="1">32.620</entry><entry morerows="1">2.7428</entry><entry morerows="1">5</entry></row><row><entry morerows="1">30</entry><entry morerows="1">33.360</entry><entry morerows="1">2.6837</entry><entry morerows="1">6</entry></row><row><entry morerows="1">31</entry><entry morerows="1">35.140</entry><entry morerows="1">2.5517</entry><entry morerows="1">4</entry></row><row><entry morerows="1">32</entry><entry morerows="1">37.060</entry><entry morerows="1">2.4238</entry><entry morerows="1">7</entry></row><row><entry morerows="1">33</entry><entry morerows="1">38.000</entry><entry morerows="1">2.3660</entry><entry morerows="1">8</entry></row><row><entry morerows="1">34</entry><entry morerows="1">39.440</entry><entry morerows="1">2.2828</entry><entry morerows="1">5</entry></row><row><entry morerows="1">35</entry><entry morerows="1">39.760</entry><entry morerows="1">2.2652</entry><entry morerows="1">6</entry></row><row><entry morerows="1">36</entry><entry morerows="1">31.540</entry><entry morerows="1">2.1721</entry><entry morerows="1">5</entry></row><row><entry morerows="1">37</entry><entry morerows="1">42.680</entry><entry morerows="1">2.1167</entry><entry morerows="1">5</entry></row><row><entry morerows="1">38</entry><entry morerows="1">43.240</entry><entry morerows="1">2.0906</entry><entry morerows="1">5</entry></row><row><entry morerows="1">39</entry><entry morerows="1">44.380</entry><entry morerows="1">2.0395</entry><entry morerows="1">10</entry></row><row><entry morerows="1">40</entry><entry morerows="1">48.340</entry><entry morerows="1">1.8813</entry><entry morerows="1">7</entry></row></tbody></tgroup></table></tables>2θ衍射角的误差为±0.2。
地址 300203 天津市河西区大沽南路敬重里4号3层